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SB 408124

Catalog #: 1963
2 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
1963/10
SB 408124 | CAS No. 288150-92-5 | OX1 Receptor Antagonists
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Description: Selective non-peptide OX1 antagonist

Chemical Name: N-(6,8-Difluoro-2-methyl-4-quinolinyl)-N'-[4-(dimethylamino)phenyl]urea

Purity: ≥98%

Product Details
Citations (2)
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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

SB 408124 is a selective non-peptide orexin OX1 receptor antagonist (Kb values are 21.7 and 1405 nM for human OX1 and OX2 receptors respectively). Blocks orexin-A induced grooming following oral administration in vivo.

Technical Data

M.Wt:
356.37
Formula:
C19H18F2N4O
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at RT
CAS No:
288150-92-5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline

Background References

  1. Dual hypocretin receptor antagonism is more effective for sleep promotion than antagonism of either receptor alone.
    Morairty SR, Revel FG, Malherbe P
    PLoS ONE, 2012;7(7):e39131.
  2. Intramolecular fluorescence resonance energy transfer (FRET) sensors of the orexin OX1 and OX2 receptors identify slow kinetics of agonist activation.
    Xu TR, Ward RJ, Pediani JD
    J. Biol. Chem., 2012;287(18):14937-49.
  3. Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor.
    Langmead et al.
    Br.J.Pharmacol., 2004;141:340
  4. Advances in novel 7-TM receptors: non-peptide orexin-1 antagonists.
    Porter
    Royal Society of Chemistry Meeting., 2001;

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Citations for SB 408124

The citations listed below are publications that use Tocris products. Selected citations for SB 408124 include:

2 Citations: Showing 1 - 2

  1. The Orexin-A-Regulated Akt/mTOR Pathway Promotes Cell Proliferation Through Inhibiting Apoptosis in Pancreatic Cancer Cells.
    Authors: Suo Et al.
    Front Endocrinol (Lausanne)  2018;9:647
  2. Orexins/hypocretins acting at Gi protein-coupled OX 2 receptors inhibit cyclic AMP synthesis in the primary neuronal cultures.
    Authors: Urbałska Et al.
    BMC Cancer  2012;46:42561

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